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ORGANIC SPECTROSCOPY

Read all about Organic Spectroscopy on ORGANIC SPECTROSCOPY INTERNATIONAL 

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DR ANTHONY MELVIN CRASTO Ph.D

DR ANTHONY MELVIN CRASTO Ph.D

DR ANTHONY MELVIN CRASTO, Born in Mumbai in 1964 and graduated from Mumbai University, Completed his Ph.D from ICT, 1991,Matunga, Mumbai, India, in Organic Chemistry, The thesis topic was Synthesis of Novel Pyrethroid Analogues, Currently he is working with AFRICURE PHARMA, ROW2TECH, NIPER-G, Department of Pharmaceuticals, Ministry of Chemicals and Fertilizers, Govt. of India as ADVISOR, earlier assignment was with GLENMARK LIFE SCIENCES LTD, as CONSUlTANT, Retired from GLENMARK in Jan2022 Research Centre as Principal Scientist, Process Research (bulk actives) at Mahape, Navi Mumbai, India. Total Industry exp 32 plus yrs, Prior to joining Glenmark, he has worked with major multinationals like Hoechst Marion Roussel, now Sanofi, Searle India Ltd, now RPG lifesciences, etc. He has worked with notable scientists like Dr K Nagarajan, Dr Ralph Stapel, Prof S Seshadri, etc, He did custom synthesis for major multinationals in his career like BASF, Novartis, Sanofi, etc., He has worked in Discovery, Natural products, Bulk drugs, Generics, Intermediates, Fine chemicals, Neutraceuticals, GMP, Scaleups, etc, he is now helping millions, has 9 million plus hits on Google on all Organic chemistry websites. His friends call him Open superstar worlddrugtracker. His New Drug Approvals, Green Chemistry International, All about drugs, Eurekamoments, Organic spectroscopy international, etc in organic chemistry are some most read blogs He has hands on experience in initiation and developing novel routes for drug molecules and implementation them on commercial scale over a 32 PLUS year tenure till date Feb 2023, Around 35 plus products in his career. He has good knowledge of IPM, GMP, Regulatory aspects, he has several International patents published worldwide . He has good proficiency in Technology transfer, Spectroscopy, Stereochemistry, Synthesis, Polymorphism etc., He suffered a paralytic stroke/ Acute Transverse mylitis in Dec 2007 and is 90 %Paralysed, He is bound to a wheelchair, this seems to have injected feul in him to help chemists all around the world, he is more active than before and is pushing boundaries, He has 100 million plus hits on Google, 2.5 lakh plus connections on all networking sites, 100 Lakh plus views on dozen plus blogs, 227 countries, 7 continents, He makes himself available to all, contact him on +91 9323115463, email amcrasto@gmail.com, Twitter, @amcrasto , He lives and will die for his family, 90% paralysis cannot kill his soul., Notably he has 38 lakh plus views on New Drug Approvals Blog in 227 countries......https://newdrugapprovals.wordpress.com/ , He appreciates the help he gets from one and all, Friends, Family, Glenmark, Readers, Wellwishers, Doctors, Drug authorities, His Contacts, Physiotherapist, etc He has total of 32 International and Indian awards

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Enzomenib


Enzomenib

CAS 2412555-70-3

MF C33H43FN6O3 MW 590.7 g/mol

5-fluoro-2-[4-[7-[(1S,3S,4R)-5-methylidene-2-azabicyclo[2.2.2]octane-3-carbonyl]-2,7-diazaspiro[3.5]nonan-2-yl]pyrimidin-5-yl]oxy-N,N-di(propan-2-yl)benzamide

5-fluoro-2-[(4-{7-[(1S,3S,4R)-5-methylidene-2-azabicyclo[2.2.2]octane-3-carbonyl]-2,7-
diazaspiro[3.5]nonan-2-yl}pyrimidin-5-yl)oxy]-N,Ndi(propan-2-yl)benzamide
menin-MLL (mixed-lineage leukemia) protein, interaction inhibitor, antineoplastic, DSP-5336, Fast Track,  Orphan Drug designations

Enzomenib is an investigational new drug that is being evaluated for the treatment of acute leukemia.[1] It is a small molecule inhibitor that targets the interaction between menin and mixed-lineage leukemia (MLL) proteins.[2] Enzomenib particularly in patients with KMT2A (MLL) rearrangements or NPM1 mutations.[3]

The U.S. Food and Drug Administration (FDA) has granted both Fast Track and Orphan Drug designations to Enzomenib.[4]

Enzomenib is an orally bioavailable, small molecule inhibitor of menin, with potential antineoplastic activity. Upon oral administration, enzomenib targets and binds to the nuclear protein menin, thereby preventing the interaction between the two proteins menin and menin-mixed lineage leukemia (MLL; myeloid/lymphoid leukemia; KMT2A) and the formation of the menin-MLL complex. This reduces the expression of downstream target genes and results in an inhibition of the proliferation of MLL-rearranged leukemic cells. The menin-MLL complex plays a key role in the survival, growth, transformation and proliferation of certain kinds of leukemia cells.

PAT

US10815241, Example 6

https://patentscope.wipo.int/search/en/detail.jsf?docId=US295244745&_cid=P21-MGISYZ-31333-1

Example 3 to 19

      The following compounds of Examples 3 to 19 were prepared according to a similar method to Example 1 by using each corresponding starting compound.
      

PAT

Optically active azabicyclo derivatives

Publication Number: JP-7614262-B2

Priority Date: 2018-08-27

Grant Date: 2025-01-15

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References

  1.  “Enzomenib – Sumitomo Pharma”AdisInsight. Springer Nature Switzerland AG.
  2.  Dempke WC, Desole M, Chiusolo P, Sica S, Schmidt-Hieber M (September 2023). “Targeting the undruggable: menin inhibitors ante portas”Journal of Cancer Research and Clinical Oncology149 (11): 9451–9459. doi:10.1007/s00432-023-04752-9PMC 11798168PMID 37103568.
  3.  “Sumitomo Pharma Presents New Clinical Data on DSP-5336 at the European Hematology Association 2024 Congress”Sumitomo Pharma Co., Ltd. 14 June 2024.
  4.  Flaherty C (15 July 2024). “FDA Grants Fast Track Designation to DSP-5336 in KMT2A/NMP1+ AML”OncLive.
Clinical data
Other namesDSP-5336
Identifiers
IUPAC name
CAS Number2412555-70-3
PubChem CID146430058
DrugBankDB18514
ChemSpider129534736
UNIIVW83Y2JLZ5
ChEMBLChEMBL5314915
Chemical and physical data
FormulaC33H43FN6O3
Molar mass590.744 g·mol−1
3D model (JSmol)Interactive image
SMILES
InChI

//////////enzomenib, Interaction inhibitor, antineoplastic, DSP 5336, Fast Track,  Orphan Drug designations